Browsing by Author "Ghardaly I.A."

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    Design and synthesis of thiazol derivatives with biological evaluations as antitumor agents
    (Bentham Science Publishers B.V., 2015) El-Sharkawy K.A.; El-Brrati M.M.A.; Ghardaly I.A.; Ali M.; Mohareb, R.M., Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt; Abdo, N.Y.M., Chemistry Department, Faculty of Education, Alexandria University, Alexandria, 21526, Egypt; El-Sharkawy, K.A., Department of Pharmaceutical Chemistry, College of Pharmacy, Jazan University, P.O. Box 114, Jazan, 45142, Saudi Arabia, Department of Chemistry, Faculty of Biotechnology, October University for Modern Sciences and Arts (MSA), El-Wahat Road, 6th October City, Cairo, Egypt
    Background: Among the wide range of heterocycles, tetrahydrobenzothienopyridine derivatives acquired a special attention due to their wide range of pharmacological activities especially the therapeutic activities. Many pharmacological drugs containing the thiophene nucleus were known in the market. Method: A series of tetrahydrobenzothienopyridine derivatives were synthesized from the reaction of 2-amino- 3-benzoyl-4,5-dihydrobenzo[b]thiophen-6(7H)-one, synthesized and used for further heterocyclization reactions through reaction with different reagents. Results: Antiproliferative evaluations and c-Met kinase, Pim-1 kinase inhibitions were performed where some compounds revealed high activities. Conclusion: The inhibition of the newly synthesized compounds towards c-Met kinase, the five c-Metdependent cancer cell lines (A549, HT-29, MKN-45, U87MG, and SMMC-7721) and one c-Met-independent cancer cell line (H460) were investigated using foretinib as a standard drug. The results showed that compounds 6b, 7e, 9b, 9e, 16c and 20d were more active than foretinib. Furthermore, compounds 6b, 13b, 16b and 16c were selected to examine their Pim-1 kinase inhibition activity, where compounds 16b and 16c were of high potencies with IC50 values of 0.28 and 0.32 ?M, while compounds 6b and 13b were less effective (IC50 > 10 ?M). � 2018 Bentham Science Publishers.